Transition metal‐catalyzed C−H bond activation has proved to be a powerful weapon for the synthesis and functionalization of privileged class of heterocycles. The 2‐aryl benzoazole (benzothiazoles, benzoxazoles and benzimidazoles) derivatives have surfaced in the scientific community with their potential applications in medicinal chemistry, agrochemistry and material science. The contribution of C−H activation strategies towards the functionalization of relevant 2‐aryl benzoazoles has been amenable in the drug discovery process. This review envelopes a decade account of the C−H activation strategies adopted for the functionalization of 2‐aryl benzoazoles.